GW4064作为法尼醇X受体激动剂的新型杂环支架
Novel heterocyclic scaffolds of GW4064 as farnesoid X receptor agonists.
作者信息
Smalley Terrence L, Boggs Sharon, Caravella Justin A, Chen Lihong, Creech Katrina L, Deaton David N, Kaldor Istvan, Parks Derek J
机构信息
Muscle Metabolism DPU, Metabolic Pathways & Cardiovascular Discovery Performance Unit, GlaxoSmithKline, Inc., Five Moore Drive, Research Triangle Park, NC 27709, United States.
Muscle Metabolism DPU, Metabolic Pathways & Cardiovascular Discovery Performance Unit, GlaxoSmithKline, Inc., Five Moore Drive, Research Triangle Park, NC 27709, United States.
出版信息
Bioorg Med Chem Lett. 2015 Jan 15;25(2):280-4. doi: 10.1016/j.bmcl.2014.11.050. Epub 2014 Nov 26.
The farnesoid X receptor (FXR) may play a crucial role in a number of metabolic diseases and, as such, could potentially serve as a target for the development of therapeutics as a treatment for those diseases. Previous work has described GW4064 as an FXR agonist with an interesting activity profile. This manuscript will describe the synthesis of novel analogs of GW4064 and the activity profile of those analogs.
法尼醇X受体（FXR）可能在多种代谢性疾病中发挥关键作用，因此，它有可能成为开发治疗这些疾病的疗法的靶点。先前的研究将GW4064描述为一种具有有趣活性特征的FXR激动剂。本手稿将描述GW4064新型类似物的合成及其类似物的活性特征。
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